Relative Bioavailability and Bioequivalence Evaluation of Bicalutamide Tablets

Pharmacokinetics characteristic and relative bioavailability of the bicalutamide test and reference tablets in healthy body was studied.With the crossover testing methods,a single oral dose of the bicalutamide test and reference tablets were given to 18 healthy volunteers.The concentrations of bicalutamide in plasma were determined by high performance liquid chromatography(HPLC),and the concentration-time curves were drawn.The major pharmacokinetic parameters and relative bioavailability of the test and reference tablets were calculated by a pharmacokinetical program,at the same time the bioequivalence of two formulations were evaluated.The result are as follows:Tmax=(4.94±0.24)h and (3.11±0.32)h,Cmax=(3885.19±1924.55)ng/mL and(4319.88±2250.15)ng/mL,t1/2=(12.59±3.31)h and (13.45±3.90)h,AUC0→48=(37966.35±9228.13)ng·h·mL-1 and(36552.52±9591.71)ng·h·mL-1,AUC0→∞=(41451.43±10326.81)ng·h·mL-1 and(40286.27±11573.62)ng·h·mL-1,respectively.The analysis showed that the 90% confidence intervals of AUC0→48 and AUC0→∞ of bicalutamide test both fell within the range from 80% to 125% of bicalutamide reference.The relative bioavailability of bicalutamide tablets was (104.85±9.62)%.Although the test tablets reached the peak more slowly than the reference tablets,no significant differences were found between T and R.Therefore,it could be considered that bicalutamide test and reference tablets are bioequivalent.